Active substanceOndansetronOndansetron
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  • Dosage form: & nbsp
    • tablets, film-coated 4 mg, 8 mg
    • solution for intravenous and intramuscular injection 2 mg / ml
    Composition:Each tablet, film-coated, 4 mg contains:

    Active ingredient: ondansetron hydrochloride dihydrate 5 mg, equivalent to ondansetron 4 mg. Excipients: corn starch 20 mg, microcrystalline cellulose (Ultra-102) 85 mg, lactose 13 mg, silicon dioxide colloid 1 mg, magnesium stearate 1 mg; composition of the membrane: hypromellose (15 cps) 2 mg, propylene glycol 0.25 mg, titanium dioxide 0.5 mg, talc 0.25 mg.

    Each tablet is film-coated. 8 mg contains:

    Active ingredient: ondansetron hydrochloride dihydrate 9.976 mg, equivalent to ondansetron 8 mg. Additives: corn starch 40 mg, microcrystalline cellulose (Ultra-102) 170,024 mg, lactose 26 mg, silicon dioxide colloid 2 mg, magnesium stearate 2 mg; composition of the membrane: hypromellose (15 cps) 4 mg, propylene glycol 0.5 mg, titanium dioxide 1 mg, talc 0.5 mg.

    1 ml of the solution contains:

    Active ingredient: ondansetron hydrochloride dihydrate 2,494 mg, equivalent to ondansetron 2 mg. Excipients: citric acid monohydrate 0.5 mg, sodium citrate 0.25 mg, sodium chloride 9 mg, water for injection up to 1 ml.
    Description:

    Tablets, film-coated 4 mg and 8 mg

    Round, biconvex tablets, film-coated, white or almost white with embossing "Rx"on one side and a smooth surface on the other side.

    Solution for intravenous and intramuscular and administration

    Transparent colorless liquid.

    Pharmacotherapeutic group:Antiemetic, serotonin receptor antagonist.
    ATX: & nbsp

    A.04.A.A.01   Ondansetron

    Pharmacodynamics:

    Ondansetron is a selective antagonist of the 5HT3 (serotonin) receptor. Medicines for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which, by activating the vagal afferent fibers containing 5НТз-receptors, causes a vomiting reflex. Selectively blocks serotonin 5HT3 receptors of neurons of the central and peripheral nervous system, endings n.vagus in the intestine and in the centers of the central nervous system (mainly the bottom of the IV ventricle), which regulate the exercise of vomitive reflexes. Does not disrupt the coordination of movements, does not cause sedation and reduced efficiency. It has anxpolitic activity. Does not change the concentration of prolactin in the plasma.

    Pharmacokinetics:

    After ingestion, the time to reach the peak concentration in the plasma (TCmah) - 1.5 hours After intramuscular injection TCmah - 10 minutes.Binding to plasma proteins is 70-76%. Metabolized in the liver with the participation of microsomal enzymes (cytochrome CYP2D6). Both after oral administration, and after parenteral administration, the elimination half-life (T1/2) is 3 hours. The absence of an enzyme CYP2D6 (debrisoquine polymorphism) does not affect the pharmacokinetics of ondansetron.

    In unchanged form, less than 5% of the administered dose is excreted in the urine.

    The pharmacokinetic parameters of ondansetron do not change with its repeated administration.

    In patients with moderate renal insufficiency (creatinine clearance 15-60 ml / min), both systemic clearance and volume of distribution are reduced, resulting in a small and clinically insignificant increase in T1 /2- The pharmacokinetics of ondansetron practically does not change in patients with severe renal dysfunction in chronic hemodialysis (studies were conducted in between hemodialysis sessions). In patients with severe impairment of liver function, the systemic clearance of ondansetron drastically decreases, resulting in an increase in the half-life of it to 15-20 hours. T1/2 ondansetron does not depend on the mode of administration.

    In elderly patients after oral administration or parenteral administration T1 /2 can increase up to 5 hours.

    Indications:

    - prevention and elimination of nausea and vomiting caused by cytotoxic chemotherapy or radiotherapy;

    - prevention and elimination of nausea and vomiting in the postoperative period.
    Contraindications:

    - increased sensitivity to ondansetron or other components of the drug.

    - pregnancy and the period of breastfeeding.

    - children under 2 years old

    Dosing and Administration:

    Cytostatic therapy

    The choice of dosage regimen is determined by the emetogenicity of antitumor therapy.

    For of adults the daily dose, as a rule, is 8-32 mg, the following regimens are recommended:

    With moderately-emetogenic chemotherapy or radiotherapy:

    - 8 mg of ondansetron 1-2 hours prior to the start of the main therapy, followed by taking another 8 mg orally after 12 hours.

    - 8 mg intravenously struino slowly or intramuscularly, immediately before the start of therapy;

    With highly emeticogenic chemotherapy:

    - The recommended dose is 24 mg concomitantly with dexamethasone inside at a dose of 12 mg 1-2 hours before the start of chemotherapy.

    To prevent late or prolonged vomiting that occurs after 24 hours, continue taking ondansetron 8 mg twice daily for 5 days.

    - 8 mg intravenously struino slowly just before the start of chemotherapy, and then two more intravenous injections of 8 mg, each of which is carried out in 2-4 hours;

    - continuous 24-hour infusion of the drug at a dose of 24 mg at a rate of 1 mg / h;

    - 16-32 mg, diluted in 50-100 ml of the appropriate infusion solution, as a 15-minute infusion, immediately before the start of chemotherapy.

    The efficacy of ondansetron can be increased by a single intravenous injection of glucocorticosteroid preparations (eg, 20 mg dexamethasone) prior to chemotherapy.

    Fly

    Children older than 2 years of the drug is administered at a dose of 5 mg / m2 the surface of the body intravenously, immediately before the start of chemotherapy, followed by ingestion of 4 mg after 12 hours; treatment is recommended to continue at a dose of 4 mg 2 times a day inside for 5 days.

    Prevention of postoperative nausea and vomiting

    Adults injected a single dose of 4 mg intramuscularly or intravenously (slowly) at the onset of anesthesia or administered 16 mg orally 1 hour prior to the onset of general anesthesia.

    For relief of nausea and vomiting it is recommended intramuscular or slow intravenous injection of 4 mg of the drug.

    Intramuscularly in the same body region ondansetron can be administered at a dose not exceeding 4 mg!

    Children to prevent postoperative nausea and vomiting ondansetron is used exclusively parenterally in a single dose of 0.1 mg / kg (maximum to 4 mg) in the form of a slow intravenous injection before or after anesthesia.

    To treat the development of postoperative nausea and vomiting in children, a slow intravenous injection of a single dose of the drug is recommended 0.1 mg / kg (maximal to 4 mg).

    In the prevention and treatment of postoperative nausea and vomiting in children under 2 years of age, there is no sufficient experience.

    Elderly patients Dosage adjustments are not required.

    Patients with violation ofFunctions kidneys

    Change the usual daily dose and the frequency of administration of the drug is not required. Patients with impaired hepatic function

    With moderate or severe impairment of liver function, the clearance of ondansetron is significantly reduced, while the half-life of it is increased from the plasma, so it is not recommended for such patients to prescribe more than 8 mg of ondansetron per day

    To dilute the injection solution, the following solutions can be used:

    0.9% solution of sodium chloride;

    5% dextrose solution; Ringer's solution;

    0.3% potassium chloride solution and 0.9% sodium chloride solution;

    0.3% potassium chloride solution and 5% dextrose solution.

    Side effects:

    Allergic reactions: urticaria, bronchospasm, laryngospasm, angioedema, anaphylaxis.

    From the digestive system: hiccough, dry mouth, constipation or diarrhea, sometimes an asymptomatic transient increase in serum aminotransferase activity.

    From the side of the cardiovascular system: pain in the chest, in some cases with depression of the segment S-T, arrhythmias, bradycardia, lowering blood pressure.

    From the nervous system: headache, dizziness, spontaneous movement disorders and convulsions.

    Local reactions: hyperemia, pain, burning at the injection site.

    Other: "tide" of blood to the skin of the face, a feeling of heat, a temporary violation of visual acuity, hypokalemia, hypercreatinemia.

    Overdose:

    In cases of suspected overdose, symptomatic therapy is indicated.

    The specific antidote is unknown.In case of an overdose of ondansetron, the use of ipecacuanas is not recommended, as it is unlikely that this drug will be effective during the antiemetic activity of ondansetron.

    Interaction:

    As ondansetron is metabolized by the enzyme system (cytochrome P450) of the liver, caution is required when combined:

    - with enzymatic inducers P450 (CYP2D6 and CYP3A) - barbiturates, carbamazepine, carisoprodol, glutethimide, griseofulvin, dinitrogen oxide, papaverine, phenylbutazone, phenytoin (probably other hydantoins), rifampicin, tolbutamide;

    - with inhibitors of enzymes P450 (CYP2D6 and CYP3A) - allopurinol, macrolide

    antibiotics, antidepressants (MAO inhibitors), chloramphenicol, cimetidine,

    estrogen-containing oral contraceptives, diltiazem, disulfiram, valproic acid and its salts, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil.

    Ondansetron at a concentration of 16-160 μg / ml is pharmaceutically compatible, and can

    be introduced through Yinjector intravenously drip, together with the following drugs:

    - cisplastin (at a concentration of up to 0.48 mg / ml) for 1-8 hours;

    - 5-fluorouracil (at a concentration of up to 0.8 mg / ml at a rate of 20 ml / h - higher concentrations may cause precipitation of ondansetron);

    - carboplatin (at a concentration of 0.18-9.9 mg / ml for 10-60 min);

    -ethoposide (in the concentration of 0.14-0.25 mg / ml for 30-60 minutes);

    - ceftazidime (in a dose of 0.25-2.0 g, as an intravenous bolus injection for 5 minutes);

    - cyclophosphamide (in a dose of 0.1-1.0 g, as an intravenous bolus injection for 5 minutes);

    - doxorubicin (at a dose of 10-100 mg, as an intravenous bolus injection for 5 minutes);

    - dexamethasone: possible intravenous administration of 20 mg dexamethasone slowly, for 2-5 minutes. The drug can be administered through a single dropper, while in a solution, dexamethasone concentrations can range from 32 μg to 2.5 mg / ml, ondansetron

    - from 8 μg to 0.1 μg / ml.

    Special instructions:

    Patients who had previously had allergic reactions to other selective 5HT3-receptor blockers have an increased risk of developing them against ondansetron.

    Ondansetron can slow the motility of the large intestine, and therefore its appointment to patients with signs of intestinal obstruction requires regular monitoring.Safety of ondansetron during pregnancy is not established.

    The infusion solution should be prepared immediately before use. If necessary, the ready-made infusion solution can be stored for up to 24 hours at a temperature of 2-8 ° C at normal illumination.

    During the infusion, protection from light is not required; The diluted injection solution retains its stability for at least 24 hours under natural light or normal light.

    Form release / dosage:A solution for intravenous and intramuscular injection of 4 mg / 2 ml or 8 mg / 4 ml (2 mg / ml) in ampoules of colorless glass.
    Packaging:

    • For 4 or 10 tablets in a strip. 1 strip with instructions for use in a cardboard bundle.
    • 2 ampoules per PVC / aluminum blister. For 1 blister, along with instructions for use in a cardboard bundle.
    • For 5 ampoules in PVC / aluminum blister. For 2 or 10 blisters together with instructions for use in a cardboard bundle.

    Storage conditions:

    List B.

    In a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children!

    Shelf life:

    3 of the year.

    The drug should not be used after the expiry date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N009021 / 02
    Date of registration:12.12.2008
    The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India
    Information update date: & nbsp18.05.2012
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